GNE-490
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CAS No. | 1033739-92-2 | Cat. No. | BCP21623 |
Name | GNE-490 | ||
Synonyms | GNE490;GNE 490; | ||
SMILES | OC(C)(C)C1=CC2=C(S1)C(N3CCOCC3)=NC(C4=C(C)N=C(N)N=C4)=N2 | ||
Chemical Name | |||
Formula | C18H22N6O2S | M. Wt | 386.47 |
Purity | 98% | Storage | Store at 4-8°C |
Description | GNE-490 is a highly selective pan-PI3K inhibitor that demonstrates selectivity over mTOR. It has good pharmacokinetic (PK) parameters and demonstrates knock down of pathway markers in vivo. Originally obtained via modification of compounds like GDC-0941, GNE-490 which have a significantly reduced potency mTOR while maintaining effective potency for PI3K substrates. IC50 values for PI3K family members are in the subnanomolar to low nanomolar range (-.28 to <20nm) while IC50 values for mTOR and other related tyrosine kinases are greater than 750 nM with most being greater than 1 uM or more, thus GNE-490 makes a good choice for examining PI3K related events separate from those mediated by mTOR. |
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